PPARgamma coactivator 1beta/ERR ligand 1 is an ERR protein ligand, whose expression induces a high-energy expenditure and antagonizes obesity

Proc Natl Acad Sci U S A. 2003 Oct 14;100(21):12378-83. doi: 10.1073/pnas.2135217100. Epub 2003 Oct 6.

Abstract

A well balanced body energy budget controlled by limitation of calorie uptake and/or increment of energy expenditure, which is typically achieved by proper physical exercise, is most effective against obesity and diabetes mellitus. Recently, peroxisome proliferator-activated receptor (PPAR) gamma, a member of the nuclear receptor, and its cofactors have been shown to be involved in lipid metabolism and in the control of energy expenditure. Here we show that PPARgamma coactivator 1 (PGC-1) beta functions as ERRL1 (for ERR ligand 1), which can bind and activate orphan ERRs (estrogen receptor-related receptors) in vitro. Consistently, PGC-1beta/ERRL1 transgenic mice exhibit increased expression of the medium-chain acyl CoA dehydrogenase, a known ERR target and a pivotal enzyme of mitochondrial beta-oxidation in skeletal muscle. As a result, the PGC-1beta/ERRL1 mice show a state similar to an athlete; namely, the mice are hyperphagic and of elevated energy expenditure and are resistant to obesity induced by a high-fat diet or by a genetic abnormality. These results demonstrate that PGC-1beta/ERRL1 can function as a protein ligand of ERR, and that its level contributes to the control of energy balance in vivo, and provide a strategy for developing novel antiobesity drugs.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • DNA / genetics
  • ERRalpha Estrogen-Related Receptor
  • Energy Metabolism
  • Gene Expression
  • Ligands
  • Mice
  • Mice, Transgenic
  • Molecular Sequence Data
  • Obesity / genetics
  • Obesity / prevention & control
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Receptors, Estrogen / metabolism*
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*

Substances

  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Estrogen
  • Recombinant Proteins
  • Transcription Factors
  • peroxisome-proliferator-activated receptor-gamma coactivator-1
  • DNA